Description

Simple

A medication used to relieve pain in the muscles and joints.

Clinical

A topical analgesic agent used for the symptomatic relief of neuropathic pain associated with post-herpetic neuralgia, as well as other muscle and joint pain.

Overview

Capsaicin is most often used as a topical analgesic and exists in many formulations of cream, liquid, and patch preparations of various strengths; however, it may also be found in some dietary supplements. Capsaicin is a naturally-occurring botanical irritant in chili peppers, synthetically derived for pharmaceutical formulations. The most recent capsaicin FDA approval was Qutenza, an 8% capsaicin patch dermal-delivery system, indicated for neuropathic pain associated with post-herpetic neuralgia.

Pharmacology

Indication

The capsaicin 8% patch is indicated in the treatment of neuropathic pain associated with post-herpetic neuralgia. There are multiple topical capsaicin formulations available, including creams and solutions, indicated for temporary analgesia in muscle and join pain as well as neuropathic pain.

Pharmacodynamic

Capsaicin is a TRPV1 receptor agonist. TRPV1 is a trans-membrane receptor-ion channel complex activated by temperatures higher than 43 degrees Celsius, pH lower than 6, and endogenous lipids. When activated by a combination of these factors, the channel can transiently open and initiate depolarizati... Read more

Mechanism of action

Capsaicin has been shown to reduce the amount of substance P associated with inflammation - however this is not believed to be its main mechanism in the relief of pain [ Read more

Absorption

**Oral**: Following oral administration, capsaicin may be absorbed by a nonactive process from the stomach and whole intestine with an extent of absorption ranging between 50 and 90%, depending on the animal [ Read more

Protein binding

Information currently not available.

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

Following oral ingestion of equipotent dose of 26.6 mg of pure capsaicin, the half life was approximately 24.9 ± 5.0 min [ Read more

Route of elimination

It is proposed that capsaicin mainly undergoes renal excretion, as both the unchanged and glucuronide form. A small fraction of unchanged compound is excreted in the feces and urine. _In vivo_ animal studies demonstrates that less than 10 % of an administered dose was found in faces after 48 h [ Read more

Toxicity

Acute oral LD50 and dermal LD50 in mouse are 47.2 mg/kg and >512 mg/kg, respectively [MSDS]. Capsaicin is shown to be mutagenic for bacteria and yeast [MSDS].

Capsaicin can cause serious irritation, conjunctivitis and lacrimation via contact with eyes. It induces a burning sensation and pain in c... Read more

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The serum concentration of (R)-warfarin can be increased when it is combined with Capsaicin.
(S)-Warfarin
The serum concentration of (S)-Warfarin can be increased when it is combined with Capsaicin.
4-hydroxycoumarin
The metabolism of 4-hydroxycoumarin can be decreased when combined with Capsaicin.
6-O-benzylguanine
The metabolism of 6-O-benzylguanine can be decreased when combined with Capsaicin.
8-azaguanine
The metabolism of Capsaicin can be decreased when combined with 8-azaguanine.
8-chlorotheophylline
The metabolism of 8-chlorotheophylline can be decreased when combined with Capsaicin.
9-aminocamptothecin
The metabolism of 9-aminocamptothecin can be decreased when combined with Capsaicin.
9-Deazaguanine
The metabolism of Capsaicin can be decreased when combined with 9-Deazaguanine.
9-Methylguanine
The metabolism of Capsaicin can be decreased when combined with 9-Methylguanine.
Abatacept
The metabolism of Capsaicin can be increased when combined with Abatacept.
Abiraterone
The serum concentration of Capsaicin can be increased when it is combined with Abiraterone.
Acebutolol
Capsaicin may increase the bradycardic activities of Acebutolol.
Acefylline
The metabolism of Acefylline can be decreased when combined with Capsaicin.
Acenocoumarol
The serum concentration of Acenocoumarol can be increased when it is combined with Capsaicin.
Acetaminophen
The metabolism of Capsaicin can be decreased when combined with Acetaminophen.
Acetylcholine
The risk or severity of adverse effects can be increased when Capsaicin is combined with Acetylcholine.
Aclidinium
The therapeutic efficacy of Aclidinium can be decreased when used in combination with Capsaicin.
Acyclovir
The metabolism of Capsaicin can be decreased when combined with Acyclovir.
Adalimumab
The metabolism of Capsaicin can be increased when combined with Adalimumab.
Afelimomab
The metabolism of Capsaicin can be increased when combined with Afelimomab.
5 References
  1. 1 . Anand P, Bley K: Topical capsaicin for pain management: therapeutic potential and mechanisms of action of the new high-concentration capsaicin 8% patch. Br J Anaesth. 2011 Oct;107(4):490-502. doi: 10.1093/bja/aer260. Epub 2011 Aug 17.PubMed: 21852280
  2. 2 . Wallace M, Pappagallo M: Qutenza(R): a capsaicin 8% patch for the management of postherpetic neuralgia. Expert Rev Neurother. 2011 Jan;11(1):15-27. doi: 10.1586/ern.10.182.PubMed: 21158551
  3. 3 . Simpson DM, Estanislao L, Brown SJ, Sampson J: An open-label pilot study of high-concentration capsaicin patch in painful HIV neuropathy. J Pain Symptom Manage. 2008 Mar;35(3):299-306. Epub 2007 Oct 23.PubMed: 17959343
  4. 4 . O'Neill J, Brock C, Olesen AE, Andresen T, Nilsson M, Dickenson AH: Unravelling the mystery of capsaicin: a tool to understand and treat pain. Pharmacol Rev. 2012 Oct;64(4):939-71. doi: 10.1124/pr.112.006163.PubMed: 23023032
  5. 5 . Oleoresin Capsicum Toxicology Evaluation and Hazard Review Link